JP6158077B2 - Piroxicam for preventive and therapeutic measures of herpes infection - Google Patents

Description

  The present invention relates to medicaments for preventive and therapeutic measures of viral infections, for example herpes infections, particularly including herpes simplex.

  Treatment of viral infections in humans and animals has always been a very difficult task, as only a limited number of agents are available, which is also true for the herpesvirus family.

  The family of herpesviridae includes a large number of viruses with double-stranded DNA. Widely prevalent are HSV type 1 and HSV type 2 herpes simplex viruses and herpes varicella zoster virus VZV. Both cause painful infections in the form of superficial inflammation. Because herpesviruses are latent in the human body for a long time, the onset of the disease can occur repeatedly and even severe symptoms can appear.

  Herpes simplex infections initially affect the mouth and develop in the form of blisters and trauma to the mucous membranes and lips. Varicella zoster infection occurs mainly in the form of chickenpox in childhood and in the form of shingles in adults. The latter leads to painful rashes in the area of the spinal nerve, for example in the area of the hips, chest, and even on the face. Shingles infections are accompanied by fever, loss of appetite, pain in the extremities, and the rash site hurts.

  Various drugs have been developed against herpesviruses, but these are mainly effective in symptom relief and generally have only a limited impact on the course of the disease. In many cases, the use of the drug only slightly shortens the duration of the disease. A frequently used agent is acyclovir.

  In short, there is a need for drugs suitable for effectively combating viral infections, particularly herpes infections.

  The publication EP 1457202A2 describes the use of so-called non-steroidal anti-inflammatory drugs (NSAIDs) for the treatment of herpes infections. Although the application mentions a very wide variety of NSAIDs, only two members of this group have been described for their effectiveness: diclofenac and ketorolac, and substantial evidence based on reliable data Only diclofenac is shown. According to the data, locally administered diclofenac is suitable for alleviating the course of the disease, and wound healing appears to take an average of 5 days. This means that the situation was unsatisfactory for the patient, although the duration of 10 days or less, the duration of normal infection, could be shortened.

Surprisingly, it has now been found that piroxicam, an agent belonging to the group of NSAIDs, is suitable for preventive and therapeutic measures of viral infections. Piroxicam has a positive effect on each case of various viral diseases, eg influenza caused by H ₁ N ₁ influenza virus, and in particular herpes infections, ie those of HSV type 1 and HSV type 2, especially Suitable for preventing cold sores or providing a rapid healing process. Piroxicam (4-hydroxy-2-methyl-N-pyridin-2-yl-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide) is a COX inhibitor and is used as an anti-rheumatic drug Yes.

  The present invention therefore relates to a medicament of the above kind containing piroxicam in a suitable carrier material.

According to the invention, the medicament is preferably 0.1-10% by weight , 0 . It is contained in an amount of 1 to 5% by weight, particularly preferably in an amount in the range of 0.5 to 5% by weight. The drug can be administered topically, orally or parenterally.

  The medicament according to the invention is advantageously used for the treatment of infections in the mouth area, generally known by the term labial herpes. This is an infection caused by HSV type 1 and HSV type 2 herpes simplex viruses, and the drug is also effective against herpes zoster VZV. All of the above infections cause superficial painful rashes.

  In general, the medicament is administered topically, in particular in the form of a cream, ointment or tincture. These usually contain carrier substances, which are formulations for creams, ointments, gels and tinctures established for clinical use.

  Furthermore, the medicament can be administered in the form of tablets, powders, infusions or injectable solutions.

  The drug is used 1 to 5 times per patient once or twice a day. The majority of patients state that a single use of the drug has been successful.

  Many patients, often suffering from herpes simplex infection, have reported that the development of such rash has been prevented by administering the drug in a stress situation that typically causes the development of herpes rash .

Test report 1
The drug according to the invention was tested against 42 subjects using a commercially available piroxicam gel having an active substance content of 0.5% by weight. The results are as follows:

  Of the 42 subjects, 26 subjects used the drug once and 16 subjects used the drug 5 times or less.

  Of the 42 subjects, 15 subjects showed signs of recovery in less than 1 day (this included preventing the onset of the disease), and 21 subjects in 1 to 3 days Recovery was reported and 2 subjects reported recovery in 4-10 days. Regarding the tolerability of the drug, 41 subjects reported good and one subject reported not so well. One subject reported that the drug did not help.

  The effectiveness of piroxicam was actually unexpected. Originally developed as an anti-rheumatic drug, chemically formally called 4-hydroxy-2-methyl-N (2-pyridinyl) -2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide Active substances are also administered as analgesics. From a chemical point of view, this is completely different from the above mentioned NSAIDs, diclofenac and ketorolac,-based on its chemical structure-antiviral activity against herpes viruses, especially herpes simplex / labial herpes I don't get it. In contrast to diclofenac and ketorolac, the drug is suitable for preventing the development of a rash.

Test report 2
In a screening test, a piroxicam-containing gel with an active substance content of 0.4% was tested against cultures infected with HSV type 1 herpesvirus using standard test methods. The first CD ₅₀ value determined was 2.50, and the virus titer was initially 7.00. The virus titer (log ₁₀ TCID ₅₀ / ml) determined after a residence time of 1.5 and 60 minutes was less than 2.50, which corresponds to a reduction in virus count of more than 99.99%. It is.

Claims (5)

A drug for preventing and treating viral infections caused by viruses from the family of herpesviridae, wherein the drug contains 0.1-10% by mass of piroxicam as a virucidal agent in a carrier substance , or injection virucidal agent, characterized in der Rukoto for.   The drug according to claim 1, wherein the content of piroxicam is 1 to 5% by mass.   The drug according to claim 1 or 2, wherein the viral infection is an infection caused by herpes simplex.   The medicine according to claim 3, wherein the herpes simplex is cold sore.   5. A medicament according to any one of claims 1 to 4 for topical administration.